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Oral pharmaceutical compositions in timed-release particle form and fast-disintegrating tablets containing this composition

Inactive Publication Date: 2005-12-29
ASTELLAS PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0014] In light of these circumstances, the inventors performed intense studies focusing on the fact that means for coating core particles containing a drug with two layers that clearly have different roles may be effective. As a result, they discovered that the above-mentioned three objectives can be simultaneously accomplished with an oral pharmaceutical composition in particle form with a multi-layered structure, which comprises particles that contain a drug at the core of the pharmaceutical composition in particle form; a middle layer that contains two types of water-soluble components, an insolubilizer and an insolubilizing substance; and an outer layer for controlling water penetration that contains a water-insoluble substance. That is, they discovered that when a pharmaceutical composition in particle form is obtained by coating core particles containing a drug with a middle layer that will not dissolve for a certain time and will quickly dissolve thereafter and further coating these particles with a layer that controls the amount of water penetration by controlling the speed with which water penetrates inside the pharmaceutical compositions, it is possible to have a sufficiently long lag time and to release drug quickly after the lag time, and it is possible to control lag time to within a length of 2 to 20 minutes by varying the amount of coating and the components of each coating layer.
[0015] Consequently, the first characteristic of the present invention is a middle layer made from a water soluble substance that will quickly dissolve after a lag time but will remain insoluble for a specific time. Thus far, a balance between lag time formation and fast drug release has been pursued using a combination of a water-insoluble substance and a water-soluble substance. However, the inventors considered that the use of a combination wherein one water-soluble substance renders insoluble another water-soluble substance is in some way related to the solution to the above-mentioned objectives. That is, the inventors believed that a layer that suppresses drug dissolution is temporarily formed by dissolution of one water-soluble substance (insolubilizer) to promote insolubilization of the other water-soluble substance (insolubilizing substance) and then once the insolubilizer was completely released, the insolubilizing substance will recover the original water solubility thereof, making fast drug release possible.

Problems solved by technology

However, the salting out-type insolubilizer and salting out-type insolubilizing substance both are very water soluble, and it was therefore estimated that even when a pharmaceutical composition in particle form is coated with this insolubilizer and this substance, both will quickly dissolve and it will not be possible to suppress initial drug release.

Method used

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  • Oral pharmaceutical compositions in timed-release particle form and fast-disintegrating tablets containing this composition
  • Oral pharmaceutical compositions in timed-release particle form and fast-disintegrating tablets containing this composition
  • Oral pharmaceutical compositions in timed-release particle form and fast-disintegrating tablets containing this composition

Examples

Experimental program
Comparison scheme
Effect test

working example 1

[0136] [Preparation of Core Particles Containing a Drug]

[0137] A liquid of 225.0 g of acetaminophen (Yoshitomi Fine Chemicals, Ltd.) and 22.5 g of hydroxypropylmethylcellulose 2910 (Shin-Etsu Chemical Co., Ltd., TC-5E, the same hereafter) dissolved in a mixture of 750.0 g of methanol (Kanto Kagaku, the same hereafter) and 653.0 g of methylene chloride (Kanto Kagaku, the same hereafter) was sprayed from the side onto 750.0 g of sucrose spheres (Freund GmbH; Nonpareil 103 (24-32)) at a product temperature of 30° C., liquid feed rate of 20 g / mL, and spraying air pressure of 2.5 kg / cm using a fluidized bed granulator (Glatt GmbH; GPCG-1, the same hereafter) to obtain core particles containing a drug.

[0138] [Preparation of Middle Layer Coating Liquid]

[0139] 44.2 g of hydroxypropylmethylcellulose 2910 were dissolved in a mixture of 1052.0 g of methanol and 450.8 g of methylene chloride, 221.0 g of sodium carbonate (Kanto Kagaku, the same hereafter) pulverized with a jet mill pulverizer (...

working example 2

[0146] [Preparation of Coating Liquid for Controlling Water Penetration]

[0147] 25.0 g of cetanol were dissolved in 975.0 g of methylene chloride to prepare the coating liquid for the layer for controlling water penetration.

[0148] [Preparation of Particles Coated with Middle Layer and Layer for Controlling Water Penetration]

[0149] The above-mentioned coating liquid for a layer for controlling water penetration was sprayed from the side onto 500.0 g of particles coated with a middle layer obtained in Working Example 1 at a product temperature of 30° C., liquid feed rate of 15 g / min, and a spraying air pressure of 2.0 kg / cm2 using a fluidized bed granulator to obtain particles coated with a middle layer and a layer for controlling water penetration wherein the particles coated with a middle layer were coated with a 5 wt % layer for controlling water penetration. The average particle diameter of the resulting particles coated with a middle layer and( a layer for controlling water penet...

working example 3

[0150] [Preparation of Middle Layer Coating Liquid]

[0151] 39.8 g of hydroxypropylmethylcellulose 2910 were dissolved in a mixture of 946.8 g of methanol and 405.8 g of methylene chloride, 198.9 g of sodium dihydrogen phosphate dihydrate (Kanto Kagaku, the same hereafter) pulverized with a jet mill pulverizer were added, and the product was stirred to prepare the middle layer coating liquid.

[0152] [Preparation of Particles Coated with Middle Layer]

[0153] The above-mentioned middle layer coating liquid was sprayed from the side onto 450.0 g of core particles containing a drug obtained in Working Example 1 at a product temperature of 30° C., liquid feed rate of 22.0 g / min, and a spraying air pressure of 4.5 kg / cm2 using a fluidized bed granulator to obtain particles coated with a middle layer wherein core particles containing a drug were coated with a 53 wt % middle layer. The average particle diameter of the resulting particles coated with a middle layer was 889 μm.

[0154] [Preparati...

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Abstract

The present invention relates to an oral pharmaceutical composition in particle form, which comprises particles that contain a drug at the core of the pharmaceutical composition in particle form; a middle layer that contains two types of water-soluble components, an insolubilizer and an insolubilizing substance; and an outer layer for controlling water penetration that contains a water-insoluble substance. The present invention makes it possible to provide a pharmaceutical composition in particle form for oral use with which initial drug release is suppressed, the drug is quickly released thereafter, and lag time can be controlled as needed, and fast-disintegrating tablets containing this composition.

Description

TECHNICAL FIELD [0001] The present invention relates to an oral pharmaceutical composition in timed-release particle form and fast-disintegrating tablets containing this composition. In further detail, the present invention relates to an oral pharmaceutical composition in particle form with a multi-layered structure, which comprises particles that contain a drug at the core of the pharmaceutical composition in particle form; a middle layer that contains two types of water-soluble components, an insolubilizer and an insolubilizing substance; and an outer layer for controlling water penetration that contains a water-insoluble substance, this oral pharmaceutical composition in timed-release particle form being such that a layer for controlling water penetration controls the speed at which water penetrates to inside the particles and an insolubilizer makes it possible to temporarily prevent dissolution of an insolubilizing substance, as well as fast-disintegrating tablets containing thi...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K9/16A61K9/20A61K9/26A61K9/50A61K31/135A61K47/02A61K47/04A61K47/10A61K47/12A61K47/18A61K47/24A61K47/26A61K47/32A61K47/34A61K47/36A61K47/38A61K47/40A61K47/42
CPCA61K9/2077A61K9/2095A61K9/5078A61K31/135A61K9/0056A61K9/5047A61K9/501A61K9/5015A61K9/5026A61K9/5042A61K9/2081A61P1/04A61P1/08A61P11/10A61P13/02A61P19/10A61P21/02A61P23/02A61P25/00A61P25/02A61P25/06A61P25/08A61P25/16A61P25/20A61P25/22A61P25/24A61P29/00A61P3/02A61P3/10A61P31/04A61P35/00A61P3/06A61P5/00A61P5/38A61P9/00A61P9/04A61P9/06A61P9/08A61P9/12
Inventor YOSHIDA, TAKAYUKITASAKI, HIROAKIKATSUMA, MASATAKAMAEDA, ATSUSHI
Owner ASTELLAS PHARMA INC
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